5-HT1B receptor

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5-hydroxytryptamine (serotonin) receptor 1B, G protein-coupled
4IAR.png
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols HTR1B ; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12
External IDs OMIM182131 MGI96274 HomoloGene669 IUPHAR: 5-HT1B ChEMBL: 1898 GeneCards: HTR1B Gene
RNA expression pattern
PBB GE HTR1B 210799 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 3351 15551
Ensembl ENSG00000135312 ENSMUSG00000049511
UniProt P28222 P28334
RefSeq (mRNA) NM_000863 NM_010482
RefSeq (protein) NP_000854 NP_034612
Location (UCSC) Chr 6:
78.17 – 78.17 Mb
Chr 9:
81.63 – 81.63 Mb
PubMed search [1] [2]

5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the HTR1B gene.[1][2] The 5-HT1B receptor is a 5-HT receptor subtype.[3]

Tissue distribution and function[edit]

5-HT1B receptors are widely distributed throughout the CNS with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus.[4] The function of the 5-HT1B receptor differs depending upon its location. In the frontal cortex, it is believed to act as a postsynaptic receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, evidence suggests 5-HT signaling acts on an autoreceptor, inducing the release of serotonin[5] and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency,[6] respectively. In the hippocampus, a recent study has demonstrated that activation of postsynaptic 5-HT1B heteroreceptors produces a facilitation in excitatory synaptic transmission which is altered in depression.[7] When the expression of 5-HT1B in human cortex is traced throughout life, A significant changes during adolescence was observed, in a way that is strongly correlated with the expression of 5-HT1E.[8]

Outside the brain, 5-HT1B receptor activation also has vascular effects, such as pulmonary vasoconstriction. Furthermore, blocking 5-HT1B receptor signaling decreases the number of osteoblasts, bone mass, and the bone formation rate.[9]

Knockout mice lacking the 5-HT1B gene have shown an increase in aggression and a higher preference for alcohol.[10] Under basal conditions, knockout mice present with a "normal" phenotype and an exhibit a sucrose preference (lack of sucrose preference is considered a measure of anhedonia). However, after undergoing chronic unpredictable stress treatment to induce a "depression-like" phenotype these animals do not benefit from administration of selective serotonin reuptake inhibitor (SSRIs).[7]

Ligands[edit]

Agonists[edit]

Partial agonists[edit]

Antagonists and inverse agonists[edit]

Genetics[edit]

In humans the protein is coded by the gene HTR1B.

A genetic variant in the promotor region, A-161T, has been examined with respect to personality traits and showed no major effect.[14]

See also[edit]

References[edit]

  1. ^ Jin H, Oksenberg D, Ashkenazi A, Peroutka SJ, Duncan AM, Rozmahel R, Yang Y, Mengod G, Palacios JM, O'Dowd BF (March 1992). "Characterization of the human 5-hydroxytryptamine1B receptor". J. Biol. Chem. 267 (9): 5735–8. PMID 1348246. 
  2. ^ Sanders AR, Cao Q, Taylor J, Levin TE, Badner JA, Cravchik A, Comeron JM, Naruya S, Del Rosario A, Salvi DA, Walczyk KA, Mowry BJ, Levinson DF, Crowe RR, Silverman JM, Gejman PV (February 2001). "Genetic diversity of the human serotonin receptor 1B (HTR1B) gene". Genomics 72 (1): 1–14. doi:10.1006/geno.2000.6411. PMID 11247661. 
  3. ^ "Entrez Gene: HTR1B 5-hydroxytryptamine (serotonin) receptor 1B". 
  4. ^ "5-hydroxytryptamine (serotonin) receptor 1B, G protein-coupled". Retrieved 23 Feb 2013. 
  5. ^ Pytliak M, Vargová V, Mechírová V, Felšöci M (2011). "Serotonin receptors - from molecular biology to clinical applications". Physiol Res 60 (1): 15–25. PMID 20945968. 
  6. ^ Huang CC, Yeh CM, Wu MY, Hsu KS (2013). "A single in vivo cocaine administration impairs 5-HT1B receptor-induced long-term depression in the nucleus accumbens". J. Neurochem. 125 (6): 809–21. doi:10.1111/jnc.12227. PMID 23452061. 
  7. ^ a b Cai X, Kallarackal AJ, Kvarta MD, Goluskin S, Gaylor K, Bailey AM, Lee HK, Huganir RL, Thompson SM (2013). "Local potentiation of excitatory synapses by serotonin and its alteration in rodent models of depression". Nat. Neurosci. 16 (4): 464–72. doi:10.1038/nn.3355. PMID 23502536. 
  8. ^ Shoval, G., Bar-Shira O., Zalsman G., John J. Mann and Chechik G. (2014) Transitions in the transcriptome of the serotonergic and dopaminergic systems in the human brain during adolescence. European Neuropsychopharmacology. (2014). "Transitions in the transcriptome of the serotonergic and dopaminergic systems in the human brain during adolescence". European neuropsychopharmacology 24 (7): 1123–32. doi:10.1016/j.euroneuro.2014.02.009. PMID 24721318. 
  9. ^ Yadav VK, Ryu JH, Suda N, Tanaka KF, Gingrich JA, Schütz G, Glorieux FH, Chiang CY, Zajac JD, Insogna KL, Mann JJ, Hen R, Ducy P, Karsenty G (November 2008). "Lrp5 controls bone formation by inhibiting serotonin synthesis in the duodenum". Cell 135 (5): 825–37. doi:10.1016/j.cell.2008.09.059. PMC 2614332. PMID 19041748. 
  10. ^ Hoyer D, Hannon JP, Martin GR (2002). "Molecular, pharmacological and functional diversity of 5-HT receptors". Pharmacol. Biochem. Behav. 71 (4): 533–54. doi:10.1016/S0091-3057(01)00746-8. PMID 11888546. 
  11. ^ Hudzik, TJ; Yanek, M; Porrey, T; Evenden, J; Paronis, C; Mastrangelo, M; Ryan, C; Ross, S; Stenfors, C (2003). "Behavioral pharmacology of AR-A000002, a novel, selective 5-hydroxytryptamine(1B) antagonist.". The Journal of Pharmacology and Experimental Therapeutics 304 (3): 1072–84. doi:10.1124/jpet.102.045468. PMID 12604684. 
  12. ^ Selkirk, JV; Scott, C; Ho, M; Burton, MJ; Watson, J; Gaster, LM; Collin, L; Jones, BJ; Middlemiss, DN; Price, GW (1998). "SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.". British Journal of Pharmacology 125 (1): 202–8. doi:10.1038/sj.bjp.0702059. PMC 1565605. PMID 9776361. 
  13. ^ Roberts, C; Watson, J; Price, GW; Middlemiss, DN (2001). "SB-236057-A: a selective 5-HT1B receptor inverse agonist.". CNS Drug Reviews 7 (4): 433–44. doi:10.1111/j.1527-3458.2001.tb00209.x. PMID 11830759. 
  14. ^ Tsai SJ, Wang YC, Chen JY, Hong CJ (2003). "Allelic variants of the tryptophan hydroxylase (A218C) and serotonin 1B receptor (A-161T) and personality traits". Neuropsychobiology 48 (2): 68–71. doi:10.1159/000072879. PMID 14504413. 

External links[edit]

  • "5-HT1B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading[edit]

This article incorporates text from the United States National Library of Medicine, which is in the public domain.